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A general synthetic approach to β-carboline-containing alkaloids was developed. Two consecutive palladium-mediated processes, a Sonagashira coupling and a Larock indole annulation reaction, are central to the method. The scope of the approach was investigated and found to be amenable for constructing a variety of biologically significant natural products and also for preparing substituted analogues for optimization and analysis of their biological properties.

Sequential Sonagashira and Larock Indole Synthesis Reactions in a General Strategy To Prepare Biologically Active β-Carboline-Containing Alkaloids